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Design, synthesis, and biological evaluation of benzylamino-methanone based cholesteryl ester transfer protein inhibitors.

ABSTRACT: Cholesteryl ester transfer protein (CETP) is a glycoprotein involved in transporting lipoprotein particles and neutral lipids between high-density lipoprotein (HDL) and low density lipoproteins (LDL) and therefore its a proper target for treating dyslipidemia and related disorders. Guided by our previously-reported pharmacophore and QSAR models for CETP inhibition, we synthesized and bioassayed a series of benzylamino-methanones. The most potent illustrated 30% CETP inhibition at 10 microM.

SUBMITTER: Abu Sheikha G 

PROVIDER: S-EPMC6257782 | biostudies-literature | 2010 Aug

REPOSITORIES: biostudies-literature

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Design, synthesis, and biological evaluation of benzylamino-methanone based cholesteryl ester transfer protein inhibitors.

Abu Sheikha Ghassan G   Abu Khalaf Reema R   Melhem Areej A   Albadawi Ghadeer G  

Molecules (Basel, Switzerland) 20100819 8

Cholesteryl ester transfer protein (CETP) is a glycoprotein involved in transporting lipoprotein particles and neutral lipids between high-density lipoprotein (HDL) and low density lipoproteins (LDL) and therefore its a proper target for treating dyslipidemia and related disorders. Guided by our previously-reported pharmacophore and QSAR models for CETP inhibition, we synthesized and bioassayed a series of benzylamino-methanones. The most potent illustrated 30% CETP inhibition at 10 microM. ...[more]

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